Assay Detail
Binding
CHEMBL2444609
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Binding mode characterization of 6α- and 6β-N-heterocyclic substituted naltrexamine derivatives via docking in opioid receptor crystal structures and site-directed mutagenesis studies: application of the 'message-address' concept in development of mu opioid receptor selective antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.76 | 8.96 |
| IC50 | 3 | 8.44 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL522143 | — | — | 2 | 8.96 |
| CHEMBL19019 | NALTREXONE | 4.0 | 2 | 8.73 |
| CHEMBL522201 | — | — | 2 | 8.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL522143 | — | Ki | = | 1.09 | nM | 8.96 |
| CHEMBL19019 | NALTREXONE | Ki | = | 1.85 | nM | 8.73 |
| CHEMBL522143 | — | IC50 | = | 2.29 | nM | 8.64 |
| CHEMBL522201 | — | Ki | = | 2.57 | nM | 8.59 |
| CHEMBL19019 | NALTREXONE | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL522201 | — | IC50 | = | 5.42 | nM | 8.27 |